DERIVATIVES OF BENZIMIDAZOLE, METHODS FOR THEIR PRODUCTION, APPLICATION OF THEM AS A PHARNESOID-X-RECEPTOR (FXR) AGONISTS AND PHARMACEUTICAL PRODUCTS CONTAINING THEM

摘要

1. The compounds of formula (I)! ! where R1 is C1-10 alkyl, lower alkoxy-lower alkyl, lower alkoxy-carbonyl lower alkyl, cycloalkyl, cycloalkyl lower alkyl, aryl, aryl lower alkyl, di (aryl) lower alkyl, heteroaryl, heteroaryl lower alkyl, heterocyclyl or heterocyclyl lower alkyl, where the cycloalkyl, aryl, heteroaryl or heterocyclyl group is optionally substituted with 1 to 3 substituents independently selected from the group consisting of lower alkyl, lower alkoxy, lower alkoxy-carbonyl, morpholinyl, formylamino, halo hydroxy group, fluoro lower alkyl, fluoro lower alkoxy group, lower alkyl carbonyl-N (lower alkyl), lower alkyl carbonyl-N (H), NH2, N (H, lower alkyl), N (lower alkyl) 2, carboxyl group, carbamoyl, N (H, lower alkyl) C (O) and N (lower alkyl) 2C (O); ! R2 is hydrogen or lower alkyl; ! R3 is lower alkyl, cycloalkyl, partially unsaturated cycloalkyl, aryl, aryl lower alkyl, heteroaryl, heteroaryl lower alkyl, heterocyclyl or heterocyclyl lower alkyl, wherein the aryl, heteroaryl or heterocyclyl group is optionally substituted with 1 to 3 substituents independently selected from a group including halogen, lower alkyl, lower alkoxy, lower alkoxy-carbonyl, hydroxy, fluoro-lower alkyl, fluoro-lower alkoxy, NH2, N (H, lower alkyl), N (lower alkyl) 2, lower alkyl-carbonyl- N (lower alkyl) lower alkyl carbonyl-N (H), a carboxyl group, carbamoyl, N (H, lower alkyl) C (O) and N (lower alkyl) 2C (O); ! R4 stands for! a) heteroaryl, which is optionally substituted with 1 to 3 substituents independently selected from the group consisting of neither